- Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
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The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.
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Paragraph 0952; 0957-0959
(2021/05/01)
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- Nickel-Catalyzed Dearomative Arylboration of Indoles: Regioselective Synthesis of C2- And C3-Borylated Indolines
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Indole dearomatization is an important strategy to access indolines: a motif present in a variety of natural products and biologically active molecules. Herein, a method for transition-metal catalyzed regioselective dearomative arylboration of indoles to
- Brown, M. Kevin,Crook, Phillip F.,Kuniyil, Rositha,Liu, Peng,Trammel, Grace L.
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supporting information
p. 16502 - 16511
(2021/10/20)
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- A kind of aldosterone synthase modulators method for the preparation of intermediates
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The invention discloses a method for preparing an aldosterone synthase conditioning agent intermediate. The method comprises the following steps: implementing reaction on a reaction substrate under Boc protection with hydrogen chloride and ethanol for acetal protection, directly heating to remove Boc protection without separation, implementing N-methylation reaction so as to obtain an N-methylation product, and directly removing acetal protection without separation, thereby obtaining a target product. The method is high in route reaction conversion rate and high in product purity, the product quality can be effectively ensured, and workshop production can be achieved.
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Paragraph 0028-0031
(2017/02/28)
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- Palladium catalyzed tandem alkenyl- and aryl-C-N bond formation: A cascade N-annulation route to 4-, 5-, 6- and 7-chloroindoles
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A series of trihalogenated alkenylbenzenes undergo consecutive palladium catalyzed inter- and intramolecular amination reactions to deliver a series of 1-functionalized mono-chloroindoles. 4-, 5-, 6- and 7-Chloroindoles can all be prepared; carbamates, anilines and amines can be employed as the N-nucleophile.
- Henderson, Luke C.,Lindon, Matthew J.,Willis, Michael C.
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experimental part
p. 6632 - 6638
(2010/10/03)
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- 2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
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The present invention is directed to a compound of Formula (XVI) wherein R, R2, R3, R4, R5, R6, R7 and n are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmac
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Page/Page column 76
(2008/06/13)
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